A compound based on CRBN ligand-induced ubiquitination degradation of Hsp90, its preparation method and uses

Compounds developed using PROTAC technology that target the degradation of HSP90 protein utilize CRBN ligand-induced ubiquitination, solving the side effects of existing inhibitors and achieving effective inhibition of breast cancer cells and significant degradation of HSP90 protein.

CN117736181BActive Publication Date: 2026-06-30FUJIAN MEDICAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
FUJIAN MEDICAL UNIV
Filing Date
2023-03-31
Publication Date
2026-06-30

AI Technical Summary

Technical Problem

Existing HSP90 inhibitors have side effects and are difficult to effectively reduce the content of HSP90 protein in tumor cells, thus affecting their anti-tumor effects.

Method used

Compounds targeting the degradation of HSP90 protein were developed using PROTAC technology. By inducing ubiquitination with CRBN ligands, the ubiquitin-proteasome system was utilized to specifically degrade HSP90 protein.

Benefits of technology

This compound exhibits a strong inhibitory effect on breast cancer cells and significantly degrades HSP90 protein, outperforming the existing drug AT13387 and demonstrating better anti-tumor efficacy.

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Abstract

This invention relates to a compound based on CRBN ligand-induced ubiquitination degradation of Hsp90, its preparation method and uses, as shown in X-Y-Z, where X represents the ligand of HSP90 protein, Z represents the ligand of E3 ligase, and Y represents the chain connecting X and Z. This type of compound can be used to treat or prevent tumors.
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